Formulations and methods for weight loss and body contouring

ABSTRACT

Formulations and methods for weight loss and body contouring are disclosed. An illustrative formulation comprises human chorionic gonadotrophin (hCG) and resveratrol. An illustrative method for weight loss and body contouring comprises administering hCG and resveratrol sublingually.

CROSS REFERENCE TO RELATED APPLICATION

This application is a continuation of, and claims the benefit of, U.S.application Ser. No. 13/975,619 filed on Aug. 26, 2013, entitled“FORMULATIONS AND METHODS FOR WEIGHT LOSS AND BODY CONTOURING.” The '619application claims priority to, and the benefit of, U.S. ProvisionalApplication Ser. No. 61/693,495 entitled “FORMULATION AND METHODS FORWEIGHT LOSS AND BODY CONTOURING,” filed Aug. 27, 2012. The entirecontents of all of the foregoing applications are incorporated herein byreference for all purposes.

FIELD

The present disclosure generally relates to health care, and moreparticularly, to formulations and methods for weight loss and bodycontouring.

BACKGROUND

People are increasingly concerned with physical appearances and health,which has led to a massive market for medical weight-loss, beauty, andanti-aging treatments. More traditional exercise regimens and/or dietshave not been sufficiently successful for many people, so a need existsfor formulations that promote rapid weight loss and body contouring.

Moreover, obesity in America has reached near “epidemic” proportionswith 66% of Americans considered overweight or obese. There is a paucityof effective weight loss treatments. Many subjects are not candidatesfor risky and aggressive gastric bypass or gastric banding obesitysurgery. Thus, a need exists for safe, non-surgical weight losstherapies.

SUMMARY

The present disclosure comprises formulations and methods for weightloss and body contouring. An illustrative formulation comprises humanchorionic gonadotrophin (hCG) and an antioxidant. Illustrativeantioxidants include flavonoids such as resveratrol. An illustrativemethod for weight loss and body contouring comprises prescribing oradministering a biological hormone and an antioxidant orally (e.g.,sublingually in the form of a liquid, tablet, lozenge, capsule, orspray), or transdermally (e.g., in the form of a cream, lotion, spray,solution, or skin patch). An illustrative method further comprises anexercise regimen and/or a low or very low calorie diet and a sustainedmaintenance program.

DETAILED DESCRIPTION

The disclosure includes formulations and methods for weight loss andbody contouring. Persons skilled in the art will readily appreciate thatvarious aspects of the disclosure may be realized by any number offormulations and methods configured to perform the intended functions.Stated differently, other formulations and methods may be incorporatedherein to perform the intended functions. Although the presentdisclosure may be in connection with various medical principles andbeliefs, the present disclosure should not be bound by theory.

The term “approximately,” as used in this specification and appendedclaims, refers to plus or minus 5% of the value given. The term “about,”as used in this specification and appended claims, refers to plus orminus 10% of the value given. Weight percentages provided herein arebased on a dosage of 350 IU/25 mg.

An illustrative formulation comprises one or more of: (i) a biologicalhormone; (ii) an antioxidant; and (iii) one or more optional excipients.

In various embodiments, and without wishing to be bound by theory, it isbelieved that the biological hormone may serve to assist in weight lossby targeting stored body fat for metabolism. It may further assist indecreasing hunger and enhancing “well-being”, while following a lowcalorie diet. The biological hormone may further provide regulation ofthe hypothalamus which “resets” the hunger center, thereby decreasingthe desire to overeat. An illustrative biological hormone compriseshuman chorionic gonadotrophin (hCG), yet other hormones are includedwithin the scope of the disclosure.

Persons skilled in the art will readily appreciate that a variety ofantioxidants or free radical scavengers are suitable for use inconnection with the present disclosure. In general, the term“antioxidant” as used herein includes any nutrient or chemical thatreacts with and neutralizes oxidants, free radicals or chemicals thatrelease free radicals, or otherwise prevents or minimizes damage tomolecular structures such as DNA, is suitable for use in connection withthe present disclosure. By way of example, vitamins A, C, E and B,beta-carotene, and selenium are all contemplated for use in connectionwith the present disclosure.

Other illustrative antioxidants comprise flavonoids, includingbioflavonoid antioxidants such as resveratrol. In illustrativeembodiments, resveratrol serves to counter the negative effects of ahigh calorie diet loaded with trans fats. Without wishing to be bound bytheory, it is believed that resveratrol produces a gene activationprofile similar to a calorie-restricted diet. Weight loss occursnaturally with a calorie-restricted diet. Therefore, since the geneactivation profile is similar to a calorie-restricted diet, weight lossshould occur. Again, without wishing to be bound by theory, it isbelieved that resveratrol increases mitochondria production, therebyincreasing the body's ability to burn nutrients and fats into energy andaccelerating the body's metabolism, which in turn helps to burnunnecessary fats before they get stored in the body and affect healthand weight.

An illustrative formulation comprises from about 0.001 to about 0.1%, orapproximately 0.01% by weight biological hormone. An illustrativeformulation further comprises from about 1 to about 10%, orapproximately 6% by weight antioxidant. The balance of the formulationcan be comprised of one or more optional excipients. Optionalexcipients, for example fillers, lubricants, disintegrants, flavorants,sweetening agents, medicants, preservatives, and/or colorants, may bepresent in an amount of up to about 99% by weight.

The term “filler” as used herein, is intended to mean inert substancesused as fillers, glidants, diluents or bulking agents to create thedesired bulk, flow properties, and compression characteristics in thepreparation of tablets and capsules. Such compounds include, by way ofexample and without limitation, dibasic calcium phosphate, kaolin,sucrose, mannitol, microcrystalline cellulose, powdered cellulose,precipitated calcium carbonate, sorbitol, starch, combinations thereofand other such materials known to those of ordinary skill in the art.

Fillers, as used herein, can be in granulated, compacted or agglomeratedform, and can be directly compressible; such as, directly compressiblemannitol, directly compressible sorbitol, directly compressiblemaltitol, directly compressible lactose, directly compressible sucrose,directly compressible xylose, directly compressible trehalose, directlycompressible dextrose, directly compressible lactose, directlycompressible microcrystalline cellulose and the like, and combinationsthereof. Lactose monohydrate spray dry (agglomerated form) can be usedin this formulation as a directly compressible filler. One or morefillers can be present in an illustrative formulation in an amount offrom about 5 to about 20%, or approximately 10% by weight.

The term “lubricant”, as used herein, is intended to mean substancesused in tablet formulations to reduce friction during tabletcompression. Such compounds include, by way of example and withoutlimitation, sodium stearyl fumarate, calcium stearate, magnesiumstearate, mineral oil, stearic acid, zinc stearate, combinations thereofand other such materials known to those of ordinary skill in the art.One or more lubricants can be present in an illustrative formulation inan amount of from about 1.5 to about 6%, or approximately 3% by weight.

The term “disintegrant,” as used herein, is intended to mean a compoundused in solid dosage forms to promote the disruption of the solid massinto smaller particles which are more readily dispersed or dissolved.Exemplary disintegrants include, by way of example and withoutlimitation, Pharmaburst® 500 (SPI Pharma, Inc.) (believed to becomprised of sugar alcohols (e.g., mannitol, maltitol, sorbitol,xylitol, lactitol, and isomalt), disintegrants (e.g., croscarmellose andcrospovidone) and flow agents (e.g., silicon dioxide)), crospovidone(e.g., Polyplasdone® XL10), croscarmellose (ac di sol), starches such ascorn starch, potato starch, pre-gelatinized and modified starchesthereof, sweeteners, clays, such as bentonite, microcrystallinecellulose (e.g., Avicel™), carsium (e.g., Amberlite™), alginates, sodiumstarch glycolate, gums such as agar, guar, locust bean, karaya, pectin,tragacanth, combinations thereof and other such materials known to thoseof ordinary skill in the art. In some embodiments, a disintegrant can bemixed with one or more directly compressible fillers as directlycompressible mannitol, directly compressible sorbitol, and directlycompressible microcrystalline cellulose. One or more disintegrants canbe present in an illustrative formulation in an amount of from about 60to about 80%, or approximately 70% by weight.

Suitable flavorants can include, for example, flavors, such as, naturalflavors, artificial flavors, and combinations thereof. Non-limitingexamples of flavor oils include spearmint oil, cinnamon oil, oil ofwintergreen (methyl salicylate), peppermint oil, clove oil, bay oil,anise oil, eucalyptus oil, thyme oil, cedar leaf oil, oil of nutmeg,allspice, oil of sage, mace, oil of bitter almonds, and cassia oil.Suitable flavoring agents also include, for example, artificial, naturaland synthetic fruit flavors such as vanilla, citrus oils (e.g., lemon,orange, lime, and grapefruit), and fruit essences (e.g., apple, pear,peach, grape, strawberry, raspberry, cherry, plum, pineapple, andapricot), and the like, and combinations thereof. One or more flavorantscan be present in an illustrative formulation in an amount of from about5 to about 20%, or approximately 10% by weight.

Suitable sweetening agents include nutritive sweeteners such as sucrose,glucose, fructose, glucose, trehalose, galactose, mannitol, sorbitol,xylitol and intensive sweeteners such as aspartame, acesulfame K,sucralose and NHDC. One or more sweetening agents can be present in anillustrative formulation in an amount of from about 0.02 to about 0.5%,or approximately 0.12% by weight.

In accordance with illustrative embodiments, an oral disintegratingtablet manufactured according to the methods described herein has anaverage sublingual disintegration time of less than approximately 60seconds at 37° C., or from approximately 30 to approximately 40 secondsat 37° C.

Table 1 sets forth an example of a 350 IU/25 mg oral disintegratingtablet in accordance with various embodiments.

TABLE 1 Ingredient Weight % Weight (mg) hCG Powder 0.01 0.003Resveratrol 98% Powder 6.00 1.50 Lactose Monohydrate (spray-dried) 9.592.40 Sodium Stearyl Fumarate 3.00 0.75 Pharmaburst ® 500 71.7 17.93Natural Peppermint Flavor 9.59 2.40 Sucralose 0.12 0.03

The oral disintegrating tablet set forth in Table 1 can be manufacturedby (i) accurately weighing out all the powders; (ii) sieving the powdersthrough #40 sieve in order to homogenize the particle size; (iii) mixingthe powders together using a V-blender for the appropriate mixing time(e.g., 1 hour for a batch size of 10,000 tablets); and (iv) compressingthe mixture from step (iii) to form a tablet.

By way of example and without limitation, to form a tablet as in step(iv) above, the materials can be deposited into a cavity, and one ormore punch members can then be advanced into the cavity and brought intointimate contact with the material to be pressed, whereupon compressiveforce is applied. The material is thus forced into conformity with theshape of the punches and the cavity. Hundreds, and even thousands, oftablets per minute can be formed in this fashion.

One of the most common challenges associated with tablet formulation inthe prior art is proper flow of the powder formula. In the prior art,powder flow is often improved by incorporating one or more flow agents,such as fumed silicon dioxide or silica gel. However, such flow agentsoften have a negative effect on the tablet hardness, necessitating anincreased weight percentage of fillers. In connection with the presentdisclosure, it was surprisingly found that lactose monohydrate (spraydried) alone in an amount equal to or about that set forth in Table 1,without any additional flow agent, yielded a finished product withbetter quality properties. The addition of the lactose monohydrateprovided for the proper flow, improved tablet hardness, and did notinterfere with the fast tablet disintegration. Thus, some embodiments ofthe present disclosure do not comprise silicon dioxide, colloidalsilica, gel silica, precipitated silica, or any other flow agent, or donot comprise any such flow agent in an amount greater than approximately1.05% by weight, or greater than approximately 0.5% by weight, orgreater than approximately 0.1% by weight.

Illustrative methods for weight loss and body contouring compriseprescribing or administering a biological hormone and an antioxidantorally (e.g., sublingually in the form of a liquid, tablet, lozenge,capsule, or spray), or transdermally (e.g., in the form of a cream,lotion, spray, solution, or skin patch).

One such method, in accordance with various embodiments, comprises (i)sublingually prescribing or administering a tablet comprising abiological hormone and an antioxidant; and (ii) instructing a subject tonot chew or swallow the tablet; and (iii) instructing the subject to letthe tablet dissolve completely; and (iv) instructing the subject tocontinue to leave the tablet in mouth for an additional 1-2 minutes, andthen swallow; and (v) instructing the subject to not eat, drink, brushteeth or put anything in mouth for an additional 15-20 minutes to allowthe tablet to absorb into the subject's oral mucosa.

An illustrative method further comprises an exercise regimen and/or alow or very low calorie diet and a sustained maintenance program. Onesuch method, in accordance with various embodiments, comprises a “loadphase” on days 1 and 2, during which a formulation in accordance withvarious embodiments is taken by a subject in the morning and/or eveningas directed, and the subject eats as much as he/she wants, especiallyfoods that are high in fat. Days 3 to 28 comprise a “diet phase,” duringwhich the subject continues taking the formulation as directed, andbegins a reduced calorie diet. In response to the subject reachinghis/her goal weight, he/she stops (or reduces) taking the formulation,but continues the reduced calorie diet for three additional days. Afterthe three additional days, the subject begins a three week “maintenancephase,” during which he/she can add fats and proteins to his/her diet inany quantity, but continues diet modification with no sugar and nostarch.

In a clinical study, the oral disintegrating tablet set forth in Table 1was prescribed to five subjects (A-E) for one month. Each subject had aninitial weigh in, at which time the subject's body mass index (“BMI”)and waist were also both measured. Each subject was then weighed weeklyfor four weeks, at which time the subject's BMI and waist were also bothmeasured. Table 2 illustrates weight loss, BMI decrease, and waistmeasurement decrease from initial weigh in to final weigh in after fourweeks.

TABLE 2 Subject A B C D E Average Weight (lbs.) 32.2 27.0 32.2 21.0 22.026.9 BMI (%) 3.90 3.60 4.40 2.80 3.30 3.60 Waist Measurement (in.) 3.56.5 3.0 3.5 3.0 3.9

No negative side effects were observed for any of the five subjects.Thus, and as supported by the data in Table 2, formulations inaccordance with various embodiments can provide for safe, non-surgicalweight loss therapies.

Systems and methods are provided. In the detailed description herein,references to “various embodiments”, “one embodiment”, “an embodiment”,“an example embodiment”, etc., indicate that the embodiment describedmay include a particular feature, structure, or characteristic, butevery embodiment may not necessarily include the particular feature,structure, or characteristic. Moreover, such phrases are not necessarilyreferring to the same embodiment. Further, when a particular feature,structure, or characteristic is described in connection with anembodiment, it is submitted that it is within the knowledge of oneskilled in the art to affect such feature, structure, or characteristicin connection with other embodiments whether or not explicitlydescribed. After reading the description, it will be apparent to oneskilled in the relevant art(s) how to implement the disclosure inalternative embodiments.

Moreover, where a phrase similar to ‘at least one of A, B, and C’ or ‘atleast one of A, B, or C’ is used in the claims or specification, it isintended that the phrase be interpreted to mean that A alone may bepresent in an embodiment, B alone may be present in an embodiment, Calone may be present in an embodiment, or that any combination of theelements A, B and C may be present in a single embodiment; for example,A and B, A and C, B and C, or A and B and C.

The foregoing disclosure is merely illustrative of the presentdisclosure and is not intended to be construed as limiting theinvention. Although one or more embodiments of the invention have beendescribed, persons skilled in the art will readily appreciate thatnumerous modifications could be made without departing from the spiritand scope of the present disclosure. By way of example, a formulation inaccordance with the present disclosure can comprise, consist essentiallyof, or consisting of, any combination of the ingredients describedabove. As such, it should be understood that all such modifications areintended to be included within the scope of the disclosure.

We claim:
 1. A formulation for weight loss consisting essentially of: human chorionic gonadotrophin in an amount of from about 0.001 to about 0.1 weight percent; resveratrol in an amount of from about 1 to about 10 weight percent; lactose monohydrate (spray-dried) in an amount of from about 5 to about 20 weight percent; sodium stearyl fumarate in an amount of from about 1.5 to about 6 weight percent; a disintegrant in an amount of from about 60 to about 80 weight percent; a flavorant; and a sweetening agent, wherein the formulation is configured to be administered orally in the form of a tablet; wherein the formulation does not comprise silicon dioxide, colloidal silica, gel silica, precipitated silica, or any other flow agent, in an amount greater than approximately 1.05% by weight; and wherein an average disintegration time is less than approximately 60 seconds at about 37° C.
 2. The formulation of claim 1, wherein: the human chorionic gonadotrophin is present in an amount of about 0.01 weight percent; the resveratrol is present in an amount of about 6 weight percent; the lactose monohydrate (spray-dried) is present in an amount of about 10 weight percent; the sodium stearyl fumarate is present in an amount of about 3 weight percent; and the disintegrant is present in an amount of about 70 weight percent.
 3. The formulation of claim 1, wherein the flavorant comprises natural peppermint flavor.
 4. The formulation of claim 3, wherein the flavorant comprises natural peppermint flavor in an amount of about 10 weight percent.
 5. The formulation of claim 1, wherein the sweetening agent comprises sucralose.
 6. The formulation of claim 5, wherein the sweetening agent comprises sucralose in an amount of about 0.1 weight percent.
 7. The formulation of claim 1, wherein the average disintegration time is from approximately 30 seconds to approximately 40 seconds at about 37° C. 